Antivirals Flashcards

(85 cards)

1
Q

fusion inhibitors for treatment of retrovirus (HIV)

A

enfuvirtide, maraviroc

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2
Q

nucleoside reverse transcriptase inhibitors for treatment of retrovirus

A

zidovudine, didanosine, lamivudine, stavudine, abacavir

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3
Q

non-nucleoside reverse transcriptase inhibitors for treatment of retrovirus

A

nevirapine, delavirdine, efavirenz

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4
Q

integrase inhibitor for treatment of retrovirus

A

raltegravir

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5
Q

nucleotide inhibitor for treatment of retrovirus

A

tenofovir

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6
Q

protease inhibitors for treatment of retrovirus

A

atazanavir, saquinavir, ritonavir, lopinavir, indinavir, nelfinavir

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7
Q

treatments for herpes simplex and varicella zoster

A

acyclovir, valacyclovir, famciclovir, penciclovir

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8
Q

treatments for cytomegalovirus

A

ganciclovir, valganciclovir, cidofovir, foscarnet

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9
Q

treatments for hep B and C

A

lamivudine, adefovir, interferon alpha, ribavirin, boceprevir, telaprevir, tenofovir

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10
Q

uncoating inhibitors for treatment of influenza

A

amantadine, rimantadine

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11
Q

viral release inhibitors for treatment of influenza

A

zanamivir, oseltamivir

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12
Q

HAART

A

highly active antiretroviral therapy

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13
Q

36 amino acid synthetic peptide, increases effectiveness of HAART in combination chemotherapy, binds to gp41 of viral envelope, prevents conformational change and impedes the fusion of the viral and host cell membranes, no cross resistance with other HIV agents, potential for resistance developing when given at suboptimal doses

A

enfuvirtide

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14
Q

a 2nd line treatment; SC; high protein binding; metabolized by proteolytic hydrolysis; injection site reactions; increased risk of bacterial pneumonia

A

enfuvirtide

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15
Q

chemokine receptor 5 antagonist; binds to CCR5 co-receptor; prevents virus from entering the host cell; oral; substrate for both CYP3A4 and P-glycoprotein; both feces and urine

A

maraviroc

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16
Q

treatment of CCR5-tropic HIV-1; in combination for patients failing other antiretrovirals, coreceptor tropism assay should be performed when a CCR5 antagonist is being considered

A

maraviroc

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17
Q

adverse effects: cough, pyrexia, rash, musculoskeletal symptoms, abdominal pain and postural dizziness, bladder irritation; possible liver and cardiac problems; interacts with CYP3A inducers and inhibitors

A

maraviroc

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18
Q

AZT (zidovudine) and 3TC (lamivudine)

A

combivir

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19
Q

AZT (zidovudine) and 3TC (lamivudine) and abacavir

A

trizivir

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20
Q

mech of action of which retroviral group: competitive inhibition of viral reverse transcriptase

A

NRTIs

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21
Q

NRTIs: analogs of pyrimidine nucleoside (T); phosphorylated to active triphosphate forms; competes w/ deoxythymidine triphosphate for incorporation into DNA

A

zidovudine and stavudine

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22
Q

NRTIs: analogs of pyrimidine nucleoside (C); compete with deoxycytidine triphosphate for incorporation into viral DNA

A

lamivudine and emtricitabine

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23
Q

NRTI: analog of purine nucleoside (A, G); active 2’,3’-dideoxyadenosine 5’-triphosphate (ddATP) competes with cellular deoxyadenosine triphosphate for incorporation into viral DNA

A

didanosine

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24
Q

NRTI: analog of purine nucleosides (G)

A

abacavir

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25
only NRTI shown to reduce perinatal HIV transmission
zidovudine
26
zidozudine is metabolized to ...
glucoronide
27
abacavir is metabolized by ...
alcohol dehydrogenase
28
which NRTI is acid labile and taken 1/2 hr before or 2 hour after meals?
didanosine
29
common toxicities of which group?: GI distress, lactic acidosis and hepatic steatosis due to mitochondrial toxicity; lipodystrophy
NRTIs
30
which NRTI can cause bone marrow suppression
zidovudine
31
which NRTI causes diarrhea, peripheral neuropathy, pancreatitis
didanosine
32
which NRTI causes peripheral neuropathy and pancreatitis
stavudine
33
which NRTI causes hypersensitivity reaction due to genetic predisposition
abacavir
34
which NRTI: avoid concurrent administration with drugs that are bone marrow suppressive
zidovudine
35
which NRTI: ganciclovir increases plasma conc 2X and methadone decreases plasma levels
didanosine
36
which NRTI: competition with zidovudine for activation enzymes
stavudine
37
which NRTI: trimethoprim-sulfamethoxazole increases plasma concentration
lamivudine
38
which NRTI: ethanol significantly increases plasma levels
abacavir
39
Tenofovir DF and emtricitadine
truvada
40
what is effective as antiretroviral chemoprophylaxis before exposure
truvada
41
mech of action of which group: bind directly to a hydrophobic pocket of the RT protein; induce conformational change in active site and block enzyme activity; do not require intracellular phosphorylation for activity
NNRTIs
42
NNRTI: CYP3A4 inhibitor
delavirdine
43
NNRTI: CYP3A4 inducers
efavirenz and nevirapine
44
which NNRTI: fever, fatigue, headache, somnolence, nausea, hepatotoxicity (elevated liver ezymes); may be severe and life-threatening
nevirapine
45
which NNRTI: neuropsychiatric (headache, dizzines, abnormal dreams), teratogenic in nonhuman primates (FDA Pregnancy Category D)
efavirenz
46
inhibits HIV-1 integrase which is needed for insertion of viral DNA into host genome; oral; glucuronidation in liver
raltegravir
47
not inducer, inhibitor or substrate of CYP3A4; metabolized by UDP glucouronosyltransferase (UGT)
raltegravir
48
what induces UGT
rifampin
49
what inhibits UGT
PI atazanavir
50
treatment of HIV as part of combination therapy and most effective ART available; effective in both acutely and chronic HIV-1 infected cells; effective in monocytes and macrophages; prevent cleavage of polyprotein and block viral maturation
protease inhibitors
51
which group: metabolized by cytochrome P-450 system; potent inhibitors of CYP3A4
protease inhibitors
52
which PI is used to increase plasma conc of other PIs
ritonavir
53
which drug lowers indinavir AUC and potentially other PIs
carbamazepine
54
which drug upregulates PIs AUC
ketoconazole
55
which drug's AUC is augmented by PIs
sildenafil
56
which PIs reduce methadone AUC
ritonavir and lopinavir
57
adverse effects of which drugs: hyperlipidemia, insulin resistance and diabetes, lipodystrophy (buffalo hump and crix-belly), gynecomastia; increased bleeding risk in hemophiliacs; increased liver function tests
PIs
58
which PI: hepatotoxicity at high doses
ritonavir
59
which PI: alopecia, kidney stones, and renal insufficiency (patients should drink 2 liters/day)
indinavir
60
which PI: hyperbilirubinemia due to inhibition of UDP glucuronosyltransferase
atazanavir
61
which group: once phosphorylated by cellular kinases have greater affinity for viral reverse transcriptase than for cellular DNA polymerase
NRTIs
62
which group: do not undergo phosphorylation and have greater affinity for viral reverse transcriptase than for cellular DNA polymerase
NNRTIs
63
which group: greater affinity for HIV aspartyl protease than for human protease
PIs
64
block DNA synthesis by inactivation of viral DNA polymerase through direct binding and competition for dNTPs and by inducing viral DNA chain termination
nucleoside analogs
65
chain terminating effect following incorporation of a nucleotide analogue
acyclovir
66
absence of viral thymidine kinase gives ... against nucleoside analogues
resistance
67
acyclic purine nucleoside analogues; indication: herpes simplex, following high IV dose: reversible renal dysfunction and neurologic toxicity
acyclovir and valacyclovir
68
acyclic purin nucleoside analogues: indications- CMV retinitis (activity 100x greater than acyclovir), oral CMV prophylaxis; adverse effect- myelosuppression
ganciclovir and valganciclovir
69
antiherpesvirus agents: oral alternative to acyclovir
penciclovir and famciclovir
70
antiherpesvirus agent: inhibits herpesvirus DNA polymerase>>human DNA polymerase; potential human carcinogen; nephotoxicity, neutropenia, ocular hypotony
cidofovir
71
a non-nucleoside anti-HSV agent; inhibits cleavage of pyrophosphate from dNTP and blocks viral DNA synthesis; effective in CMV retinitis
foscarnet
72
myelosuppressant and has teratogenic potential
ganciclovir
73
nephrotoxic
cidofovir and foscarnet
74
anti-hep agent: nucleoside analog of guanosine; inhibits all 3 activities of HBV polymerase; equally active against lamivudine-resistan HBV; HBV exacerbation upon discontinuation of treatment
entecavir
75
anti-hep agent: nucleotide analog prodrug; active against all HCV genotypes; monotherapy not recommended; once daily oral; metabolized in liver and elimination is renal; extreme caution when used in combo with ribavirin (Pregnancy category X)
sofobuvir
76
anti HBV; nucleotide analog; inhibits HBV DNA polymerase; exacerbations of hepatitis after discontinuation; lactic acidosis
adefovir
77
nucleotide reverse transcriptase inhibitor
tenofovir
78
all nucleoside analogs- lactic acidosis and severe hepatomegaly with steatosis is a more common adverse effect in the treatment of ...
HIV
79
inhibitors of transcription; potent cytokines that possess antiviral, immunomodulating and antiproliferative actions
interferons
80
3 main classes of human IFNs
alpha, beta and gamma
81
adverse effects: flu-like syndrome, nausea, vomiting, anorexia, CV abnormalities, myelosupression, neurotoxicity, hepatotoxicity, should not be administered during pregnancy
interferon alpha-2
82
nucleoside analog of guanosine; interference with synthesis of GTP and inhibits GTP 5' capping of viral mRNA; dose dependent hemolytic anemia; bone marrow suppression
ribavirin
83
NS3/4A proteas inhibitors; block serine protease; potent inhibitors of CYP3A4/5
boceprevir and telaprevir
84
antiinfluenza; inhibitors of uncoating of virus; acts on maturation of influenza HA glycoprotein' oral prophylaxis against influenza A (not B); good alternative to vaccine
amantadine, rimantadine
85
antiinfluenza; inhibitors of influenza neuraminidase; effective against influenza A and B
zanamivir, oseltamivir